LY2955303 is a potent and selective retinoic acid receptor gamma (RARγ) antagonist with a Ki of 1.09 nM.
LY2955303 is tested and observed that the binding Kis for RARα, RARβ and RARγ are >1700, >2980 and 1.09 nM, respectively. The functional Ki for RARγ is 7.1±4.9 nM[1].
A single oral dose of LY2955303 demonstrates a dose responsive effect whereby the rat reduces differential weight bearing (ED50=0.72 mg/kg)[1].
References:
[1]. Hughes NE, et al. Identification of potent and selective retinoic acid receptor gamma (RARγ) antagonists for the treatment of osteoarthritis pain using structure based drug design. Bioorg Med Chem Lett. 2016 Jul 15;26(14):3274-3277.